The invention relates to a molecule mixture comprising an amphipathic molecule of type A, which has an overall positive charge in the hydrophilic region, an amphipathic molecule of type B, and a polyphenol C, as well as to a method for producing the molecule mixture, and to the use thereof.
Polyphenols are secondary plant metabolites that occur in plant seeds, leaves and fruits. Some of these compounds have an inhibiting effect on cancer cells (Mentha, R. G., Murillo G., Naithani R. and Peng X., Pharm Res (2010) 24:950-961) or offer protection from undesirable oxidation processes (Queen B. L., Tollefsbold T. O., Curr. Aging Sci. (2010), 3:34-42). As a result, they are considered to be important constituents of human nutrition. Meanwhile, they are also important constituents in chemotherapy, since they have a toxic effect in extremely high concentrations. Given the high therapeutic relevance of polyphenols, the controlled and effective administration thereof to human beings is of great interest.
Administering such hydrophobic active ingredients in aqueous solutions has several drawbacks. First, a very high concentration is required to achieve a therapeutic effect. The majority of the active ingredient is present in a manner such that it is not accessible to the cells and, as a result, there is no cellular uptake of approximately 99% of polyphenols. Secondly, these ingredients lose their effect due to undesirable oxidation in aqueous environments.
Admittedly, liposomes and polymer capsules increase the bioavailability of polyphenols, given their more physicochemical nature and hydrophilic properties, as compared to aqueous administration (Nair H. B. at al., Biochem. Pharmacology (2010). 80:1833-1843; Kristl J. at al., Eu. J. of Pharmaceutics and Biopharmaceutics (2009). 73:253-259; Narayanan N. K., Nargi D., Randolph C., and Narayanan B. A., (2009). Int. J. Cancer, 125:1-8), While these capsules offer advantages, the drawback is that controlled delivery and fast uptake of the polyphenol by the target cells are not ensured. In addition, these liposomes can protect the polyphenol only partially against undesirable oxidation processes.